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PubMed1990

[Drug-induced esophagitis and its complications. Retrospective study of 30 case reports and review of 650 published cases (1970-1987)].

Prevalence and incidence of drug-related esophagitis are probably underestimated. The condition can often be diagnosed on the basis of history alone. Tetracyclines and emepronium bromide were implicated in most published cases. Endoscopy usually shows erosions in the upper two thirds of the esophagus. These esophageal lesions generally heal after the medication has been stopped. Complications such as stricture, hemorrhage or perforation are very rare.

Adolescent↗
PubMed1990

Drug induced esophageal lesions studied in vitro.

This paper describes an in vitro method of studying the esophago-irritant potential of oral formulations of drugs. Porcine esophagus was used. The method offers the possibility of studying muscle activity and enzyme leakage (e.g. LDH) and of performing histomorphology of the exposed preparations. Examples of drugs which were tested are alprenolol (Aptin), propranolol (Inderal), doxycycline (Idocyklin) and (Vibramycin) and emepronium bromide (Cetiprin). Concerning effects on muscle activity, Aptic caused a marginal contraction while Cetiprin caused a relaxation of the esophagus preparation. Increased LDH-leakage was noted during exposure with the above mentioned pills in comparison with concurrent control preparations. Histopathological examination disclosed morphological changes such as softening and necrosis of the squamous epithelium of the esophageal mucosa after exposure to drugs like Idocyklin and Aptin.

Alprenolol↗
PubMed1987

Medication-induced esophageal injury: survey of the literature.

A review of the 127 cases of drug-induced esophagitis reported since 1970 indicates that commonly used medications may be a source of esophageal injury. Retrosternal pain, odynophagia, and dysphagia were the most commonly reported symptoms and most cases were self-limited with 7 to 10 days of symptomatic therapy. Occasionally, severe odynophagia or dysphagia necessitated hospitalization. Emepronium bromide, tetracycline, and its derivatives, potassium chloride, and quinidine accounted for 89% of the reported cases; the remaining 11% were caused by 14 other medications. Serious sequelae, including death, have been linked to potassium-induced esophageal injury. With other medications, however, serious complications were rare. The diagnostic study of choice for suspected medication-induced esophageal injury is endoscopy, although air contrast barium swallow may often detect subtle mucosal abnormalities. In uncomplicated cases the history alone may be sufficient to make the diagnosis. Concurrent ingestion of adequate amounts of fluid and avoidance of unnecessary bedtime medications may help to prevent medication-induced esophageal injury.

Adolescent↗
PubMed1979

[Drug-induced esophageal ulcers].

In cases without a history of gastrointestinal or cardiac disease, acute odynophagia prompts the tentative diagnosis of drug-induced esophageal ulcer. Possible causes are tetracycline, clindamycin, emepronium bromide, potassium chloride, etc. Other diseases such as carcinoma can be ruled out by endoscopy and biopsy. To avoid such esophageal lesions drugs should be taken with sufficient fluid and not immediately before bedrest.

Adult↗
PubMed1978

[Treatment of motor dysfunction of the urinary bladder].

Symptoms and objective characteristics of 86 female patients with bladder instability and uninhibited detrusor contractions suffering from urgency incontinence were analyzed. The subjective and objective response to a six week-parasympathicolytic treatment with Emepronium-Bromide (Cetiprin) was examined and the results are discussed.

Adult↗
PubMed2002

Anticholinergic drugs versus placebo for overactive bladder syndrome in adults.

BACKGROUND: Around 16% of adults have symptoms of overactive bladder (urgency with frequency and/or urge incontinence). The prevalence increases with age. Anticholinergic drugs are commonly used to treat this condition. OBJECTIVES: To determine the effects of anticholinergic drugs for the treatment of overactive bladder syndrome. SEARCH STRATEGY: The Cochrane Incontinence Group trials register was searched to January 2002. SELECTION CRITERIA: Randomised or quasi-randomised trials in adults with overactive bladder syndrome that compared an anticholinergic drug with placebo treatment or no treatment. DATA COLLECTION AND ANALYSIS: Two reviewers independently assessed eligibility, trial quality and extracted data. Data were processed as described in the Cochrane Collaboration Handbook. MAIN RESULTS: Fifty one trials, 32 parallel designs and 19 crossover designs were included (6713 adults). Most trials were described as double-blind, but were variable in other aspects of quality. The crossover trials did not present data in a way that allowed inclusion in the meta-analysis. Seven medications were tested: darifenacin; emepronium bromide or carrageenate; oxybutynin chloride; propiverine; propantheline; tolterodine; and trospium chloride. One trial included the newer, slow release, formulation of tolterodine. After treatment, cure/improvement (RR 1.41, 95%CI 1.29 to 1.54), changes in leakage episodes in 24 hours (WMD -0.56, 95%CI -0.73 to -0.39), number of voids in 24 hours (WMD -0.59, 95%CI -0.83 to -0.36), maximum cystometric volume (WMD 53.85 ml, 95%CI 42.28 to 65.41), and volume at first contraction (WMD 52.25 ml, 95%CI 37.45 to 67.06), were significantly in favour of medication. Medication was associated with significantly higher residual volumes (WMD 4.06 ml, 95%CI 0.73 to 7.39) and more than two and a half times the rate of dry mouth (RR 2.61, 95% CI 2.27 to 3.00). Sensitivity analysis, while limited by small numbers of trials, showed little likelihood that these effects were modified by age, sex, diagnosis, or choice of drug. REVIEWER'S CONCLUSIONS: The use of anticholinergic drugs by people with overactive bladder syndrome results in statistically significant improvement in symptoms. However, the clinical significance of these differences is uncertain, and the longer-term effects are not known. Dry mouth is a common side effect of therapy.

Adult↗
PubMed2006

Anticholinergic drugs versus placebo for overactive bladder syndrome in adults.

BACKGROUND: Around 16% of adults have symptoms of overactive bladder (urgency with frequency and/or urge incontinence). The prevalence increases with age. Anticholinergic drugs are commonly used to treat this condition. OBJECTIVES: To determine the effects of anticholinergic drugs for the treatment of overactive bladder syndrome. SEARCH STRATEGY: We searched the Cochrane Incontinence Group Specialised Trials Register (searched 14 June 2005) and the reference lists of relevant articles. SELECTION CRITERIA: Randomised or quasi-randomised trials in adults with overactive bladder syndrome that compared an anticholinergic drug with placebo treatment or no treatment. DATA COLLECTION AND ANALYSIS: Two reviewer authors independently assessed eligibility, trial quality and extracted data. Data were processed as described in the Cochrane Handbook for Systematic Reviews of Interventions (Higgins 2005). MAIN RESULTS: Sixty -one trials, 42 with parallel-group designs and 19 crossover trials were included (11,956 adults). Most trials were described as double-blind but were variable in other aspects of quality. The crossover trials did not present data in a way that allowed inclusion in the meta-analysis. Nine medications were tested: darifenacin; emepronium bromide or carrageenate; oxybutynin; propiverine; propantheline; tolterodine; trospium chloride; and solifenacin. One trial included the newer, slow release formulation of tolterodine. At the end of the treatment period, cure or improvement (relative risk (RR) 1.39, 95% CI 1.28 to 1.51), difference in leakage episodes in 24 hours (weighted mean difference (WMD) -0.54; 95% CI -0.67 to -0.41) and difference in number of voids in 24 hours (WMD -0.69; 95% CI -0.84 to -0.54) were statistically significant favouring medication. Statistically significant but modest sized improvements in quality of life scores were reported in recently completed trials. There was three times the rate of dry mouth in the medication group (RR 3.00 95% CI 2.70 to 3.34) but no statistically significant difference in withdrawal (RR 1.11, 95% CI 0.91 to 1.36). Sensitivity analysis, while limited by small numbers of trials, showed little likelihood that the effects were modified by age, sex, diagnosis, or choice of drug. AUTHORS' CONCLUSIONS: The use of anticholinergic drugs by people with overactive bladder syndrome results in statistically significant improvements in symptoms. Recent trials suggest that this is associated with modest improvement in quality of life. Dry mouth is a common side effect of therapy but did not seem to have an effect on the numbers of withdrawals. It is not clear whether any benefits are sustained during long-term treatment or after treatment stops.

Adult↗
PubMedDate not supplied

Effects of drugs used in the therapy of detrusor hyperactivity on the volume-induced contractions of the rat urinary bladder.

In this study we examined the effects of the drugs most commonly utilized in the therapy of overactive detrusor, on the volume-induced contractions of rat urinary bladder. Anticholinergics such as propantheline bromide and emepronium bromide, as well as oxybutynin decreased the amplitude of the voiding contractions after intravenous (i.v.) administration in a dose-dependent way. These anticholinergics, on the other hand, generally increased the frequency of the contractions. Nifedipine dose-dependently reduced the amplitude of the contractions. Flavoxate induced a dose-related decrease in the frequency without effects on the amplitude of the peaks. Its main metabolite 3-methylflavone-8-carboxylic acid (MFCA) was inactive after i.v. administration. Terodiline was active on the amplitude and apparently on the frequency of the voiding contractions. The alpha-adrenoceptor antagonist prazosin, as well as indomethacin, inhibited only the frequency of the voiding contractions. All the drugs active in reducing the frequency of the voiding contractions after i.v. administration, proved effective also after intracerebroventricular (i.c.v.) injection. The model of the volume-induced contractions of rat urinary bladder, seems to be a useful tool to evaluate in vivo the effects of a compound on the bladder, allowing the possibility of distinguishing among antimuscarinics and calcium antagonists, which peripherally decrease bladder contractility, and other drugs inducing a decrease in the frequency of the voiding reflex acting on the micturition centre(s) in the central nervous system (CNS).

Animals↗
PubMedDate not supplied

Medication-induced oesophageal injury. Survey of the literature.

This is a review of the 127 cases of drug-induced oesophagitis reported in the English language literature since 1970. The most common symptoms reported were retrosternal pain, odynophagia, and dysphagia. Most cases were self-limited and symptoms resolved in 7 to 10 days with symptomatic therapy. Occasionally, severe odynophagia or dysphagia necessitated hospitalisation. Emepronium bromide, tetracycline and its derivatives, potassium chloride, and quinidine account for 89% of the reported cases of medication-induced oesophageal injury. 14 other medications have been reported to injure the oesophagus. Serious sequelae, including death, have been linked to potassium-induced oesophageal injury. With other medications, however, serious complications were rare. The diagnostic study of choice is endoscopy; an air-contrast barium swallow may also detect the often subtle mucosal abnormalities produced by medication injury. However, the diagnosis does not require confirmation by radiographical or endoscopic means in all cases, and the history alone may be sufficient to make the diagnosis in uncomplicated cases. Medication-induced oesophageal injury is preventable if pills are taken with an adequate amount of fluid and if the practice of taking medications immediately before bedtime is avoided.

Drug-Related Side Effects and Adverse Reactions↗
PubMed1991

Effects of different drugs on the cystometrogram in conscious rats.

The effects on urodynamic parameters of i.v. administration of different drugs utilized in the therapy of detrusor instability, have been studied in conscious catheterized rats. Emepronium bromide, oxybutynin and nifedipine affected in a dose-dependent way the micturition pressure (MP), with sporadic changes in bladder volume capacity (BVC). Terodiline induced significant increases in BVC values in a wide range of doses. These changes, however, were always not dose-dependent. The drug significantly reduced MP only at the higher administered dose (10 mg/kg). Flavoxate induced increases of bladder capacity (BVC) not dependent on the administered doses, with no changes in micturition pressure (MP). Indomethacin significantly increased BVC and weakly reduced MP, but the effects were not dose-related. The effects of drugs on BVC were unrelated with the basal value of this parameter, whereas the decrease of MP seems to be related to high basal values before treatment. From a quantitative point of view, cystometrographic recordings in conscious normal rats can provide comparative data among drugs acting on bladder contractility (MP) such as anticholinergics and strong calcium antagonists.

Animals↗
PubMed1990

The management of detrusor instability.

Detrusor instability is a urodynamic diagnosis made when the detrusor is shown objectively to contract, spontaneously or on provocation, during the filling phase of a cystometrogram while the patient is attempting to inhibit micturition. It often is responsible for symptoms of urgency, frequency, nocturia, urge incontinence, and nocturnal enuresis, but is not synonymous with any of them. Furthermore, it may be responsible for urinary incontinence which appears to be simple stress incontinence, and should be excluded before an operation for genuine stress incontinence is undertaken. Patients with mixed incontinence should have their detrusor instability treated before an attempt at surgical correction of stress incontinence is made. A number of therapeutic options exist for the unstable bladder. The simplest is bladder drill. My own preference is to start patients on bladder drill in conjunction with oxybutynin chloride 5 mg orally three times daily, with the plan of weaning them off the medication if possible in 3-6 months. Propantheline bromide in dosages of 15-30 mg orally four times daily also appears to be effective. Imipramine, in dosages of 25-50 mg orally twice daily, or up to 75 or 100 mg orally at night also may be helpful, especially if the patient suffers from nocturia or nocturnal enuresis. The effects of imipramine appear to be additive to those of other drugs, and this makes it a useful adjunct in therapy. Emepronium bromide and flavoxate hydrochloride appear to be less useful pharmacologic agents. The expected addition within the next few years of terodiline hydrochloride to the drugs available in the United States is likely to improve significantly our ability to treat detrusor instability. The use of prostaglandin synthetase inhibitors in women with perimenstrual exacerbations of their symptoms may be useful on a case-by-case basis. Patients who do not experience improvement with behavioral intervention and pharmacologic treatment may be candidates for electric stimulation therapy or surgery. The efficacy of electric stimulation therapy is diminished in many cases by poor patient acceptance. The most effective surgical treatment for refractory detrusor instability appears to be augmentation cystoplasty, which should be attempted only by a trained reconstructive urologist, and which should be reserved for the most refractory and difficult cases.

Female↗
PubMed1986

Perioperative autonomic hyperreflexia in high spinal cord lesions: a case report.

We report the case of a 20-year-old man with serious perioperative attacks of autonomic hyperreflexia starting during urological surgery 14 months after a complete C6-C7 spinal cord injury. The intraoperative attacks were controlled by deepening the level of anaesthesia, while the postoperative attacks were treated with emepronium bromide. A brief discussion of the pathophysiology and treatment is given.

Adult↗
PubMed1980

The treatment of patients with urinary incontinence after prostatectomy.

Seventy-seven patients were treated for incontinence after prostatectomy for benign prostatic hypertrophy. Forty-six patients had detrusor instability and 28 had stable bladders. No cause for the incontinence was found in 3 patients. The majority of the group had sphincter damage (74%). Conservative treatment other than drugs was all that was required in 22 patients, but drugs such as Eskornade, imipramine or emepronium were used in a further 19. Some symptomatic improvement occurred in 53% of these 19 patients. Surgery was required in 38 cases (relief of obstruction endoscopically in 11, insertion of prosthetic devices in 27). Endoscopic treatment rarely effected a cure, but the results with prostheses were satisfactory, a cure or improvement occurring in 65% of the patients, with a low complication rate.

Humans↗
PubMed1990

Inhibition of nicotine-induced relaxation of the bovine retractor penis muscle by compounds known to have ganglion-blocking properties.

1. The relative potency in blocking the nicotine-induced relaxation of the bovine retractor penis muscle (BRP) was estimated for 12 drugs known to have ganglion-blocking properties. 2. The order of potency of the drugs studied was mecamylamine greater than chlorisondamine greater than pentolinium greater than propantheline greater than (+)-tubocurarine greater than hexamethonium greater than emepronium greater than tetraethylammonium greater than glycopyrrolate greater than decamethonium greater than butylscopolamine greater than scopolamine. 3. The results conform well to those obtained with other pharmacological methods used for the estimation of ganglion-blocking activity. 4. It is concluded that blockade of the nicotinic relaxation of the BRP can be used as an alternative method for quantitative assessment of ganglion-blocking activity. 5. Advantages of this technique are that it discriminates well between antinicotinic and antimuscarinic activity and that it satisfies most or all ethical and economical demands. 6. It is also possible that this method has certain value in predicting whether a drug has enough ganglion-blocking activity to be likely to cause impotence.

Animals↗
PubMed1982

Non-steroidal anti-inflammatory drugs and benign oesophageal stricture.

Drug histories were obtained from 76 patients at the time of initial Eder-Puestow dilatation for benign oesophageal stricture. Six patients had consumed drugs known to cause oesophageal ulceration (emepronium bromide and potassium preparations). Of the remaining 70 patients, 22 had regularly taken a non-steroidal anti-inflammatory drug before the onset of dysphagia compared with 10 patients in a control group matched for age and sex; this difference was significant (p less than 0.02). Non-steroidal anti-inflammatory drugs may have a causative role in the formation of oesophageal stricture in patients with gastro-oesophageal reflux, in whom they should be prescribed with caution.

Administration, Topical↗
PubMed1980

Esophageal lesions caused by orally administered drugs. An experimental study in the cat.

This article presents an experimental method using cats for investigation of the local ulcerogenic properties of oral drugs in the esophagus. 15 drugs in current clinical use were tested. The drugs were placed in esophagus and the animals were sacrificed after 5--8 h, 4--7 or 21 days. The esophagus was cut open, photographed macroscopically and sectioned for light microscopy. Several drugs, e.g. doxycycline, alprenolol, propranolol, ferrosuccinate, ferrosulfate, and emepronium bromide showed marked ulcerogenic properties, whereas indomethacin and betamethasone did not cause any lesions in the cat esophagus. The results seem to be in accordance with the local effect these same drugs exert on the human esophageal mucosa. In order to predict and prevent drug-induced esophageal lesions in man we suggest that oral drugs should be tested concerning their local ulcerogenic properties in the esophagus.

Administration, Oral↗
PubMed1977

Flavoxate hydrochloride in the treatment of detrusor instability.

42 patients with 'unstable bladder' were treated with flavoxate hydrochloride. A previous treatment with parasympathicolytic drugs (propantheline bromide and/or emepronium bromide) was unsuccessful. The instability of the detrusor was proven by a urodynamical investigation. Flavoxate hydrochloride is a papaverine-like smooth muscle relaxant. The results and the complications of the treatment are discussed.

Adolescent↗
PubMed1980

Urodynamic response of unstable bladder to flavoxate.

Bladder instability provokes frequency, urgency, urge incontinence and enuresis in a great percentage of patients of both sexes, who undergo urodynamic examination when other clinical elements are not in evidence. The presence of bladder contractions of variable entity, even capable of inducing emptying, during filling are accompanied by a strong desire to micturate. Our study includes daily recordings of rhythm and quantity of micturitions and leaks, evaluation of urethral pressure, transurethral cystometry and uroflowmetry. The urethral pressure profile was performed with the technique of Brown and Wickham by infusing at 2 ml/min with 10-Ch catheter, withdrawn at a speed of 15 cm/min. Transurethral cystometry was performed by a continuous infusion at moderate speed (50 ml/min) of an isotonic solution at room temperature in a recumbent patient with two catheters in the bladder. When the contractions of the detrusor appear, we evaluate the pharmacological response to the filling with a myolitic agent (flavoxate) first, and with synthetic anticholinergic (emepronium bromide) after, with the purpose of discriminating the myogenic or neurogenic nature of the alteration and to propose suitable therapy.

Adult↗